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Pharmaceutics II Exam 2 > Topical preparations - suppositories > Flashcards

Topical preparations - suppositories Flashcards

1
Q

what type of suppositories are available

A

rectal
vaginal
urethral

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2
Q

define suppositories

A

suppositories are solid dosage forms intended for insertion into body orifices where they MELT, SOFTEN, OR DISSOLVE and exert localized OR systemic effects

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3
Q

true or false

suppositories are solid dosage forms and only provide systemic effects

A

false

they are solid dosage forms but can provide local or systemic effects

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4
Q

explain the shape, length, and mass of rectal suppositories

A

cylindrical shape
~32mm in length
~2 grams* (NO MORE THAN 2 GRAMS)

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5
Q

Explain the shape and mass of vaginal suppositories

A

pessaries, globular or cone shaped
~5 grams

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6
Q

explain the shape and mass of urethral suppositories

A

slender, pencil shaped
~4 grams

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7
Q

explain the action of local suppositories

A

the suppository base melts, softens, or dissolves and delivers the medication to the tissues of that local region

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8
Q

name 4 things in which the local action of suppositories can provide relief

A

pain
irritation
itching
inflammation

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9
Q

explain what hemorroidal suppositories are.
do they provide local or systemic effects?

A

local effects

they are local anesthetics, vasoconstrictors, astringents, analgesics, soothing emollients, and protective agents

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10
Q

what can vaginal suppositories be used for

A

contraceptives and antiseptics

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11
Q

give an example of a vaginal contraceptive and how it works

A

nonxynol-9

is a surfactant that can interact with the cell membrane and be a barrier

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12
Q

what LOCAL action can urethral suppositories have

A

antibacterials and local anesthetics

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13
Q

which type of suppositories can be used for systemic effects and why?

A

rectal and vaginal, because many drugs can be absorbed through the mucous membranes in those areas

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14
Q

name 5 advantages that systemic suppositories have over the oral route

A

-effective route for patients who have vomiting issues

-convenient route for patients or are unable or unwilling to swallow medication

-bypass hepatic first pass metabolism

-a drug that is irritating to the stomach when given orally can be given via suppository and not cause this irritation

-avoids GI incompatibility of drugs (inactivation of drugs by the pH or enzymatic activity of the stomach)

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15
Q

which have more options available to provide systemic effects – ointments, creams, or suppositories?

A

suppositories have the most

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16
Q

what is the length of the human rectum

A

15-30cm

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17
Q

how many mL of insert fluid is available for the human rectum

A

2-3mL

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18
Q

true or false

there are villi and microvilli present in the human rectum

A

FALSE – there is not

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19
Q

speak about the vascularization of the human rectum

A

there is abundant blood vascularization and lymphatic vessels

the lower hemorrhoidal veins that surround the colon receive the absorbed drug and initiate circulation throughout the body, BYPASSING THE LIVER (not 100%)
lymphatic circulation assists in the absorption

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20
Q

true or false

in the case of drug absorption from rectal suppositories, first pass effects are 100% avoided

A

FALSE

the lower hemorrhoidal veins that surround the colon receive the absorbed drug and initiate circulation throughout the body which bypasses the liver, BUT the upper region of the rectum may absorb some drug as well and go to the hepatic vein

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21
Q

what assists in drug absorption from rectal suppositories

A

lymphatic circulation

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22
Q

explain the pH and buffer capacity of the human rectum

A

the pH of the rectal fluid is around 7-8 and has NO buffer capacity

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23
Q

the pH of the human rectum is 7-8 (about neutral)
what is the benefit of this?

A

don’t have to worry about an acid-base reaction occurring and the drug is generally NOT chemically changed in the rectal environment

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24
Q

explain how colonic contents (contents of the colon) can affect drug absorption through the rectum

A

a void (empty) rectum provides greater absorption

diarrhea and colonic obstruction due to a tumor will lessen absorption

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25
what physiochemical factors must be considered with drug absorption from the rectum
the lipid-water solubility and the particle size
26
why is particle size a physiochemical factor to consider when considering drug absorption from rectal suppositories
the partition coefficient a lipophilic drug in a fatty suppository base at a low concentration will have less tendency to escape from the base and will result in LOW bioavailability because the majority of the drug will remain in the suppositiry
27
why is particle size a concern when considering the absorption of drugs from rectal suppositories
the smaller the particle size, the more readily available the drug is for absorption
28
true or false when considering rectal suppositories, it is not ideal to have the drug be very soluble in the base because the drug won't release much and bioavailability will be low
TRUE
29
Classify the suppository bases
-fatty or oleaginous -water soluble or water miscible -miscellaneous
30
explain the ideal suppository base
-bland and non irritating, chemically stable, compatible with the med, easily forms a solid by compressing or molding, remains a solid at room temp but softens, melts, or dissolves readily at body temp
31
true or false a strong drug-base interaction inhibits the release of the drug
TRUE
32
why must a suppository base be capable of melting, softening, or dissolving?
to release the medication
33
for which are we more concerned with irritation - suppositories or ointments?
suppositories bc the tissues where they're inserted are very sensitive
34
what are the most frequently used suppository bases
fatty or oleaginous bases (hydrocarbons)
35
give 5 examples of fatty/oleaginous suppository bases. which is the most popular
cocoa butter** palm kernel oil cottonseed oil glyceryl monostearate glyceryl monopalmitate
36
explain all of the properties of cocoa butter. include: -where is it obtained from -what color and state of matter -what chemical structure -what temp does it melt -what solidifying agents are included
natural product obtained from Theobroma Cacao yellowish-white solid chemically -- a triglyceride melts at 30-36 degrees C solidfiying agents: cetyl esters wax (beeswax)
37
true or false cocoa butter contains water
FALSE - does not contain water. it is a triglyceride that contains fatty acid groups
38
what is a disadvantage of cocoa butter that sometimes causes us to use PEG instead
it melts at 30-36 degrees celsius which is around our body temperature. thus, if we hold it for too long it'll start to get soft
39
give 5 advantages of PEG bases
-do not need to be formulated to melt at body temp -its melting point is considerably higher than body temp. convenient for storage -- does not need fridge -PEG bases permit slow release of the drug -easy to handle when administering -do not leak from the orifice (like many cocoa butter base suppositories)
40
name the water-soluble/water miscible suppository bases that are available in the market
glycerinated gelatin and PEG bases (carbowax)
41
true or false water soluble/water miscible suppository bases do NOT contain water
TRUE
42
which is more popular as a water soluble/water miscible suppository base - glycerinated gelatin or PEG bases
PEG is more popular
43
explain PEG suppository bases (carbowax)
mix PEG 200-600 (clear liquid) with PEG 1000 or more (wax-like, white solid) to get the desired consistency PEG 200, 400, 600, 1000, 1500, 1540, 3350, 4000, 6000, AND 8000 are used
44
explain how PEG bases are used and how they are formed
they do not melt at body temp (like cocoa butter), they dissolve slowly in the body fluids. this allows for controlled release for a prolonged period of time/ formed via FUSION METHOD (uses heat)
45
explain why glycerinated gelatin water soluble/water miscible base contains the ingredients it does
gelatin is also a component of capsules. glycerin is added to soften the gelatin
46
true or false ointment bases cannot be used for suppository bases
false - a lot can
47
true or false suppository bases do not contain water
true
48
explain the difference in storage between cocoa butter and PEG
cocoa butter must be stored in the fridge because it softens at room tmep, but PEG does not
49
true or false miscelaneous suppository bases are normally not used
true
50
name some formulation variables for suppository based
physical state particle size solubility viscosity brittleness volume contraction drug release rates special problems
51
what can the physical state of the API of the suppository base be?
can be liquid or powder
52
of the formulation variables for suppository bases, which are related to the drug itself ?
physical state particle size solubility
53
small particle size = ____solubility and ____ bioavailability
high solubility and high bioavailability
54
what are some things to consider if the drug used in the suppository are solid particles?
need to use levitation to sufficiently reduce the particle size
55
what is aspirin solubility in PEG base? what does this mean?
aspirin solubility in PEG base is LOW therefore, a little of the drug will dissolve in the PEG base and the insoluble particles will be dispersed in the base. THIS IS HOW THE RELEASE RATE IS CONTROLLED
56
how is solubility a concern when formulating suppositories
the solubility of the drug in the base used — helps to control the release rate
57
explain the ideal “brittleness” of the suppository base
it cannot be easily broken. we want to maintain ridgedness to a certain extent but not break it when inserted
58
explain the release rate of: oil-soluble drug in an oily base
slow release bc of poor escaping tendency this will provide long duration
59
explain the drug release rate of: water soluble drug in an oily base
this will provide RAPID RELEASE the solubility is bad so some drug dissolves but not a lot. thus, only a small quantity of drug is needed.
60
is this acceptable: solubility of the drug is 10mg in 100g. solubility of the drug in the base is very bad. 1 mg will provide therapeutic effect
YES it is okay. most of the drug will be able to release out because solubility is so poor
61
explain the drug release rate of: oil soluble drug in water muscle base (PEG)
MODERATE RELEASE
62
explain the drug release rate of: water miscible drug in water miscible base
moderate release — all based on diffusion all are water soluble
63
true or false when a drug dissolves in the suppository base, it can easily escape to provide therapeutic effect
FALSE the drug will remain there and not come out the INSOLUBLE PARTICLES are the ones that are able to escape
64
true or false suppositories can only contain solid/powder API
false can contain liquid API as welll
65
how is “volume contraction” a formulation consideration when preparing suppositories?
in the molding method, when the suppository is placed in the fridge some of the material changes the amount that changed depends on the drug and how much base we use
66
true or false for both suppositories and ointments, the amount of drug incorporated is usually low
true
67
true or false drug release rates only apply to suppositories
FALSE applies to ointments and suppositories
68
how many methods are there for preparation of suppositories? name them
3: molding hand rolling and shaping compression
69
explain the molding method of preparing suppositories
the base is melted. the melt is incorporated into the molds. allow the melt to cool and congeal (harden) into suppositories. remove the formed suppositories from the mold the mold must be lubricated to prevent sticking, and calibrated determining the amount of base required is challenging preparing and pouring the melt
70
name a lubricant for suppository molds
liquid petrolatum (mineral oil)
71
if you use a HIGH DENSITY DRUG, the volume occupied will be _____ what does this say about the amount of base needed
LOW therefore, a lot of base will be needed
72
which suppository base(s) can use hand rolling/shaping as a method of preparation?
ONLY for cocoa butter - not PEG. PEG is not soft enough to be able to do this and needs to be melted
73
what 2 ingredients require the use of a lubricant in the molding method?
glycerin and gelatin
74
which suppository base has the more significant volume constriction problem ?
PEG when it shrinks, it won’t stick to the mold
75
the compression method of preparing suppositories is mainly used where?
in manufacturing
76
explain the compression method of preparing suppositories. where is it mainly used?
prepared by forcing the mixed mass of the suppository based and medicaments into special molds using suppository making machines suppository base + medicaments + other ingredients undergo thorough mixing prior to this compression THE COMPRESSION PROCESS IS SUITABLE FOR WHAT KIND OF COMPONENTS -heat labile (sensitive) -suppositories containing a great deal of insoluble substances in the base
77
what suppository bases are suitable for the molding method
cocoa butter glycerinated gelatin PEG most other bases too
78
true or false basically any suppository base can use the molding method
TRUE
79
what kind of components/bases are suitable for the compression method of preparing suppositories ?
heat sensitive components and suppositories containing a lot of insoluble substances
80
true or false hand rolling/shaping CANNOT be used for cocoa butter bases
FALSE can be used for cocoa butter but not PEG because it isn’t soft enough
81
name 3 stability concerns for suppositories
physical stability chemical stability microbiological stability
82
explain microbiological stability for suppositories
-for COMPOUNDED suppositories - beyond use dating -for MANUFACTURED suppositories - expiration dating -inform and education the patient about storage - if PEG, room temp is fine. cocoa butter needs fridge. glycerin has evaporating issue — needs to be stored properly otherwise it will become brittle when evaporates
83
explain how a suppository should be inserted
-position patient on left side with upper leg flexed. lubricate the suppository with a water soluble lubricant (or small amount water) if needed. gently insert suppository a finger length deep at an angle towards umbilicus so the suppository is placed against the rectal wall for ABSORPTION, rather than being left in the canal or pushed into mass of stool after the finger is withdrawn, hold buttocks together until urge to expel has ceased
84
low particle size = _____ sedimentation
slow
85
low viscosity of the suspension = _____ sedimentation
high
86
true or false the addition of a flocculating agent will increase the sedimentation rate
true
87
true or false increasing the particle size of the active ingredient will decrease sedimentation rate
false - increase
88
true or false particles in flocculated suspensions exist as separate entities
FALSE - deflocculated
89
is the sedimentation rate high in flocculated or deflocculated suspensions?
flocculated
90
true or false talc can be used as a suspending agent
false
91
name 2 suspending agents
acacia methylcellulose
92
name 2 advantages of aerosol dosage forms
fine particle size less contamination
93
true or false aerosol dosage forms are relatively inexpensive to make
false - expensive
94
propellants used in aerosols have ___ vapor pressure at 70 degrees fahrenheit
high
95
what does high vapor pressure mean
they easily evaporate
96
true or false propellants used in aerosols may not dissolve in water
TRUE
97
true or false the propellants used in aerosols have liquid densities LOWER than water at 70 degrees fahrenheit
true
98
substances used as suppository bases that DISSOLVE rather than melt…
any PEG
99
true or false water soluble bases do not contain aqueous solution
TRUE
100
true or false absorption bases contain aqueous solution
true — when anhydrous becomes W/O emulsions
101
true or false hydrocarbon bases can be used for preparation of W/O emulsions
false
102
true or false absorption bases can be used for preparation of W/O emulsions
true
103
true or false water removable bases can be used for preparation of W/O emulsions
FALSE
104
can an aqueous solution be incorporated into white petrolatum?
no - it is hydrocarbon base
105
can aqueous solution be incorporated into vaseline?
NO - hydrocarbon
106
true or false lanolin can be used to incorporate aqueous solutions
yes — it is an absorption base
107
nitroglycerin TDDS can be compared on the basis of?
the number of mg of nitroglycerin delivered in 24 hours daily delivery amount
108
true or false Nitro-Dur contains nicotine
false - nitroglycerin
109
name some penetration enhancers for TDDS
DMS (decylmethylsulfoxide) oleic acid azone alcohol
110
are pseudoplastic flow and thixotropic flow desirable properties in pharmaceutical suspensions?
yes
111
explain a Dilatant
a liquid who’s viscosity is increased when stress is applied as you agitate, viscosity increases
112
in which type of flow are substances called “shear thinning” systems
pseduoplastic flow
113
“the flow curve begins at the origin and there is no yield value””
pseudoplastic flow
114
true or false for pseudoplastic flow, the viscosity of the substances increases with increasing shear rate
FALSE

Pharmaceutics II Exam 2 (7 decks)

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